Index of drugs

Adults: prevention of delayed nausea and vomiting after chemotherapy (CINV); prevention of nausea and vomiting associated with radiotherapy (RINV); Symptomatic treatment of nausea and vomiting, including nausea and vomiting associated with acute migraine attack - Metoclopramide can be used in combination with oral analgesics to increase the absorption of analgesics in acute migraine attacks. Children aged 15-18: prevention of delayed nausea and vomiting after chemotherapy (CINV), as a second-line drug.

1 tabl contains 10 mg of metoclopramide hydrochloride. The preparation contains lactose.

Antiemetic, stimulating peristalsis. Metoclopramide is a Dopamine receptor antagonist, a 5-HT receptor antagonist₃ and weakly stimulates the scrolls. It blocks presynaptic dopamine receptors and facilitates the release of acetylcholine from cholinergic motoneurons in the intestinal wall. Thanks to this, metoclopramide facilitates the release of acetylcholine from neurons, which acts on muscarinic M receptors₂ in smooth muscle cells of the digestive tract, inducing contraction. Facilitating physiological conduct in cholinergic neurons, Metoclopramide, in a coordinated manner, intensifies propulsive activity. Increases the tone of smooth muscles, the strength of propulsive movements and accelerates gastric emptying. In addition, the coordination of pyloric activity with relaxation of the proximal duodenum and motor function of the upper gastrointestinal tract is improved. The drug does not affect the secretion of digestive juices in the stomach, bile and pancreatic enzymes. Increases the resting tension of the lower esophageal sphincter. Almost does not work on the motility of the colon and gallbladder. It penetrates the blood-brain barrier. It has a calming and anti-emetic effect, it stops nausea. After oral administration, they are quickly and almost completely absorbed from the gastrointestinal tract. In patients with gastritis the absorption time may change. Bioavailability is 80% ± 15%. The effect of the drug begins within 30-60 minutes after application. Binding to plasma proteins is small (13-30%), mainly with albumin. Metoclopramide passes through the placental barrier and into breast milk. The concentration of the drug in milk after 2 hours after application is greater than in the plasma. Metoclopramide is only metabolised to a small extent. T_0,5 is 5-6 h and prolonged in patients with impaired renal function: is about 10 h in patients with a creatinine clearance of 10-50 ml / min and 15 h in patients with a creatinine clearance <10 ml / min. Cumulative drug accumulation was observed in patients with cirrhosis. Approx. 85% of the oral dose of the drug is excreted in the urine, mainly unchanged or bound with sulfuric acid and glucuronic acid within 72 h; the remaining amount is excreted in faeces.

Hypersensitivity to the active substance or to any of the excipients. Bleeding, obstruction or perforation of the gastrointestinal tract, where stimulation of peristalsis may be a risk. Found or suspected pheochromocytoma due to the risk of severe episodes of hypertension. Tardive dyskinesia due to a history of neuroleptic or metoclopramide. Epilepsy (increased frequency and intensity of seizures). Parkinson's disease. Simultaneous use of levodopa or dopaminergic receptor agonists. Methemoglobinemia induced by metoclopramide in interviews or deficiency of NADH cytochrome b5 reductase. Use in children under 1 year, due to the increased risk of extrapyramidal disorders.

The drug may cause extrapyramidal symptoms, especially in children and adolescents, and (or) after high doses. These reactions usually occur at the beginning of treatment and may occur after a single administration. In the event of extrapyramidal symptoms, metoclopramide should be discontinued immediately. These symptoms are usually completely reversible after discontinuation, but may require symptomatic treatment (use of benzodiazepines in children and / or drugs used in anticolinergic Parkinson's disease in adults).Observe the 6-hour interval between consecutive metoclopramide doses, even if vomiting and dose rejection, to avoid overdosing. Long-term treatment with metoclopramide may induce tardive dyskinesia, potentially irreversible, especially in elderly patients. In case of clinical symptoms of tardive dyskinesia, treatment should be discontinued. Neuroleptic malignant syndrome has been reported during treatment with metoclopramide in combination with neuroleptics and metoclopramide alone. If signs of a neuroleptic malignant syndrome appear, the use of metoclopramide should be discontinued immediately and appropriate treatment initiated. Special care should be taken in patients with neurological disorders and patients taking other medicines acting on o.u.n. Metoclopramide may exacerbate the symptoms of Parkinson's disease. Methemoglobinemia has been reported, which may be associated with a deficiency of cytochrome b5 NADH reductase. In such cases, metoclopramide should be discontinued immediately and permanently and appropriate measures should be included (eg treatment with methylene blue). Due to the risk of serious cardiovascular side effects, caution should be exercised when using metoclopramide, especially by intravenous route, in elderly patients, in patients with impaired cardiac conduction (including prolongation of QT interval), patients with uncorrected electrolyte imbalance, bradycardia and patients taking other drugs that prolong the QT interval. Hypokalaemia may occur in patients with impaired renal function. In patients with a history of depression, especially in moderate to severe conditions with suicidal tendencies, a relapse may occur during treatment with metoclopramide - before starting treatment, consider whether the potential benefits of treatment outweigh the possible risks. Metoclopramide causes a transient increase in plasma aldosterone concentration - it can cause fluid retention especially in patients with cirrhosis or congestive heart failure. Metoclopramide increases the level of prolactin, therefore caution should be exercised in patients with a history of breast cancer. This form of the drug is not suitable for children of the month. below 61 kg - other forms / strengths of the drug should be used in this group of patients. The product contains lactose - should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.

Metoclopramide can be used during pregnancy if clinically justified. The occurrence of extrapyramidal symptoms in the newborn can not be ruled out when metoclopramide is used at the end of pregnancy - avoid taking the drug at the end of pregnancy. If metoclopramide is used, birth control of the newborn should be performed. Metoclopramide is excreted in breast milk to a small extent. Adverse effects can not be excluded in breastfed infants. The use of metoclopramide during breastfeeding is not recommended. Discontinuation of metoclopramide in breast-feeding women should be considered.

Very often: drowsiness. Common: depression, extrapyramidal disorders (especially in children and young adults and (or) if the recommended dose is exceeded), symptoms of Parkinson's disease, akathisia, anxiety, fatigue and fatigue, diarrhea, asthenia, drop in blood pressure (especially after intravenous administration). Uncommon: hypersensitivity, amenorrhea, hyperprolactinemia, hallucinations, dystonia, dyskinesia, decreased level of consciousness, bradycardia (especially after intravenous administration). Rare: mellitus, confusion, insomnia, convulsions (especially in patients with epilepsy), headache and dizziness, visual disturbances, swelling of the tongue or larynx, toxic effects on the liver when used with other hepatotoxic drugs. Very rare: neutropenia, leukopenia and agranulocytosis (without a clear association with the use of metoclopramide), bronchospasm (especially in patients with a history of asthma), rash or urticaria. Frequency unknown: methaemoglobinaemia, which may be associated with a deficiency of cytochrome b5 NADH reductase (especially in newborns), sulphhemoglobinemia (mainly after the simultaneous use of high doses of sulfur-releasing preparations), anaphylactic reaction (including anaphylactic shock,especially after intravenous administration), gynecomastia, impotence, porphyria, tardive dyskinesia (may be prolonged, during or after long-term treatment, especially in elderly patients), neuroleptic malignant syndrome, cardiac arrest, shortly after administration of the drug by injection and which may occur as a result of bradycardia, atrioventricular block, sinus arrest (especially after intravenous administration), prolongation of the QT interval in the ECG record,torsade de pointes, tachycardia, shock, syncope after intravenous administration, acute hypertension in patients with pheochromocytoma, urinary incontinence or frequent urination. The following sometimes associated reactions occur at a higher frequency following the use of high doses: extrapyramidal symptoms: acute dystonia and dyskinesia, symptoms of Parkinson's disease, akathisia even after a single dose of the drug, especially in children and adolescents; drowsiness, reduced level of consciousness, confusion, hallucinations.

Orally. Adults (all indications): the recommended dose is 10 mg to 3 times a day. The maximum recommended daily dose is 30 mg or 0.5 mg / kg. The maximum recommended duration of treatment is 5 days. Prevention of delayed nausea and vomiting after chemotherapy (CINV) - children and adolescents aged 15-18 years: the recommended dose is 0.1-0.15 mg / kg. up to 3 times a day. The maximum daily dose is 0.5 mg / kg. In patients aged 15-18 years of age. above 60 kg, it is recommended to use 1 tabl. 10 mg to 3 times a day. The maximum recommended duration of treatment is 5 days. The 10 mg tablets are a form of medicine not suitable for use in children at birth. less than 61 kg. At least a 6 hour interval should be respected between each dose administered, even in case of vomiting and rejection of the dose, to avoid overdose. In elderly patients a dose reduction should be considered depending on renal and hepatic function and general health. In patients with end-stage renal disease (creatinine clearance ≤ 15 ml / min), the daily dose should be reduced by 75%. In patients with moderate or severe renal impairment (creatinine clearance 15-60 ml / min), the daily dose should be reduced by 50%. In patients with severe hepatic impairment, the dose should be reduced by 50%.